Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity.
Int J Parasitol Drugs Drug Resist
; 8(3): 459-464, 2018 12.
Article
en En
| MEDLINE
| ID: mdl-30396013
ABSTRACT
In spite of recent efforts to eradicate malaria in the world, this parasitic disease is still considered a major public health problem, with a total of 216 million cases of malaria and 445,000 deaths in 2016. Artemisinin-based combination therapies remain effective in most parts of the world, but recent cases of resistance in Southeast Asia have urged for novel approaches to treat malaria caused by Plasmodium falciparum. In this work, we present chloroquine analogs that exhibited high activity against sensitive and chloroquine-resistant P. falciparum blood parasites and were also active against P. berghei infected mice. Among the compounds tested, DAQ, a chloroquine analog with a more linear side chain, was shown to be the most active in vitro and in vivo, with low cytotoxicity, and therefore may serve as the basis for the development of more effective chloroquine analogs to aid malaria eradication.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Plasmodium berghei
/
Plasmodium falciparum
/
Diseño de Fármacos
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Cloroquina
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Antimaláricos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Int J Parasitol Drugs Drug Resist
Año:
2018
Tipo del documento:
Article
País de afiliación:
Brasil